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Molecules containing bis (heteroaryl) maleimide backbones and their use in inhibiting DDE / DDD enzymes

机译:含有双(杂芳基)马来酰亚胺骨架的分子及其在抑制DDE / DDD酶中的用途

摘要

The invention concerns molecules with a bis-(heteroaryl)maleimide structure and having inhibiting characteristics with respect to enzymes with a catalytic pocket comprising the invariant amino acids D, D and E or D, D and D, such as transposases, RAG recombinases or retroviral integrases. The invention also concerns the use of said molecules for in vitro, ex vivo or in vivo inhibition of transposases, RAG recombinases and retroviral integrases such as HIV integrase, as well as the use of said molecules in the treatment of diseases associated with these enzymes in an animal or human host, in particular in the treatment of AIDS.
机译:本发明涉及具有双(杂芳基)马来酰亚胺结构并且对于具有催化口袋的酶具有抑制特性的分子,所述催化口袋包含不变氨基酸D,D和E或D,D和D,例如转座酶,RAG重组酶或逆转录病毒整合。本发明还涉及所述分子在体外,离体或体内抑制转座酶,RAG重组酶和逆转录病毒整合例如HIV整合酶的用途,以及所述分子在治疗与这些酶相关的疾病中的用途。动物或人类宿主,尤其是在治疗艾滋病方面。

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